Cholinergics

Question 1

Nicotinic receptors have what structure and are what type of receptor?

Answer 1

Pentameric structure

Ligand-gated ion channels

Question 2

What are the major muscarinic subtypes in the body?

Answer 2

M1, M3, M5 inositol phosphate pathway

M2, M4 inhibit adenylyl cyclase (reduce cAMP)

Question 3

M1

Answer 3

CNS

Stomach

Question 4

M2

Answer 4

Cardiac muscle

CNS

Airway smooth muscle

Question 5

M3

Answer 5

Airway smooth muscle

Glandular smooth tissue

Question 6

M4/5

Answer 6

CNS

Probably other stuff people will figure in the future, be thankful we’re taking this class now..

Question 7

Nm

Answer 7

Skeletal muscle at NMJ

Question 8

Nn

Answer 8

Autonomic ganglia

Adrenal medulla

CNS

Question 9

Scopolamine and Atropine are ______ amines

Answer 9

Tertiary

Question 10

Glycopyrrolate is _____ amine

Answer 10

Quaternary

Question 11

Which antimuscarinic has the strongest antisialagogue and sedative effects?

Answer 11

Scopolamine

Question 12

Which antimuscarinic has the strongest effect on increasing HR?

Answer 12

Atropine

Question 13

Why is glycopyrrolate prefered over atropine in many cases?

Answer 13

Does not cross the BBB and thus has fewer CNS effects (little sedation)

Question 14

Glycopyrrolate vs Atropine kinetics

Answer 14

IV atropine onset is 1 minute, duration 30-60 minutes. E1/2 2.3 hrs. 18% unchanged in urine, rest is hydrolyzed.

IV glycopyrrolate onset is 2-3 minutes, duration 30-60 minutes, E1/2 1.25 hrs, 80% unchanged in urine.

Question 15

Who would see a bigger effect from atropine, an old patient or a young patient?

Answer 15

Young patient- high baseline vagal tone, this decreases as we age

Question 16

What must we always give when antagonizing NMB?

Answer 16

Anticholinesterase drug

Question 17

Ipratropium uses and dosing

Answer 17

Bronchodilation

MDI 40-80mcg 2 puffs
0.25-0.5mg via neb
30-90 minute onset time
Useful in asthmatics, COPD, and smokers prior to airway instrumentation

Question 18

We would want to avoid anticholinergics in what type of ophtho cases?

Answer 18

Narrow angle glaucoma, it increase IOP

Question 19

Anticholinergics can reduce what side effect of opioids?

Answer 19

Biliary and ureteral spasm

Question 20

Scopolamine dosing

Answer 20

0. 3-0.5mg or 5mcg/kg (pre-op)

1. 5mg transdermal (5mcg/hr x 72 hrs- nausea)

Question 21

Atropine

Answer 21

0.2-0.4mg IV (pre-op)
0.4-1.0mg IV (bradycardia)
2mg in 5ml NS via neb (bronchodilation)

Question 22

Glycopyrrolate

Answer 22

0.1mg-0.2mg IV (pre-op and bradycardia)

Question 23

Central anticholinergic syndrome is more likely to occur with ________ and __________. What are the S/S and treatment?

Answer 23

Scopolamine and atropine

Restlessness, hallucinations, somnolence, unconsciousness

Delayed emergence/recovery in PACU

Give physostigmine 15-60 mcg/kg IV as needed q1-2 hours

Question 24

Atropine doses below 0.4mg for bradycardia can actually do what?

Answer 24

Make the bradycardia worse!

Question 25

Other anticholinergics

Answer 25

Ipratropium (Atrovent), Tiotropium (Spiriva)- COPD

Oxybutynin (Ditropan), Tolterodine (Detrol)- overactive bladder (M non-specific)

Darifenacin (Enablex), Solifenacin (Vesicare)- overactive bladder (M3 specific)